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Publications Tropomyosin Receptor Kinases (Trk)

Bernard-Gauthier, V*.; Mossine, A.V.; Mahringer, A.; Aliaga, A., Bailey, J. J.*; Shao, X.; Stauff, J.; Arteaga, J.; Sherman, P.; Grand'Maison, M.; Rochon, P. L.; Waengler, B.; Waengler, C.; Bartenstein, P.; Kostikov, A.; Kaplan, D. R.; Fricker, G.; Rosa-Neto, P.; Scott, P. J. H.; Schirrmacher, R. (2018). Identification of [18F]TRACK, a fluorine-18-labeled tropomyosin receptor kinase (Trk) inhibitor for PET imaging. Journal Medicinal Chemistry (cover image February). 61(4): 1737-1743.


Mossine, A.V., Brooks, A.F., Bernard-Gauthier, V.,*, Bailey, J.J.,* Ichiishi, N., Schirrmacher, R., Sanford, M.S., Scott, P.J.H. (2018). Automated synthesis of PET radiotracers by copper-mediated 18F-fluorination of organoborons: Importance of the order of addition and competing protodeborylation. J Label Compd Radiopharm. 61(3): 228-236.


Bailey, J.*, Schirrmacher, R., Farrell, C*., Bernard-Gauthier, V*. (2017). Tropomyosin receptor kinase inhibitors: an updated patent review for 2010-2016 – Part II. Expert Opinion On Therapeutic Patents. 27(7): 831-849.


Bernard-Gauthier, V*, Bailey, J.J., Mossine, A.V., Lindner, S.K., Vomacka, L., Aliaga, A., Shao, X., Quesada, C.A., Sherman, P.S., Mahringer, A., Kostikov, A., Grand'Maison, M., Rosa-Neto, P., Soucy, J.-P., Thiel, A., Kaplan, D. R., Fricker, G., Wängler, B., Bartenstein, P., Schirrmacher, R. and Peter J. H. Scott. (2017). A Kinome-Wide Selective Radiolabeled TrkB/C Inhibitor for in Vitro and in Vivo Neuroimaging: Synthesis, Preclinical Evaluation and First-in-Human. Journal of Medicinal Chemistry (Scott and Schirrmacher share last authorship) (cover image August). 60(16): 6897-6910.


Bailey, J.*, Schirrmacher, R., Ferrell, K.*, Bernard-Gauthier, V.*. (2017). Tropomyosin receptor kinase inhibitors: an updated patent review for 2010-2016 – Part I. Expert Opinion On Therapeutic Patents. 27(6): 733-751.


Bernard-Gauthier, V.*, Vesnaver, M.*, Mahringer, A., Fricker, G., Schirrmacher, R. (2017). Design and synthesis of a fluorinated quinazoline-based typeII Trk inhibitor as a scaffold for PET radiotracer development. Bioorg Med Chem Lett. 27(12): 2771-2775.


Bernard-Gauthier, V.*, Schirrmacher, R. (2015). Evaluation of WO2015042088 A1 - a novel urea-based scaffold for TrkA inhibition. Expert Opinion on Therapeutic Patents. 26(2): 291-5.


Bernard-Gauthier, V.*, Bailey, J.J.*, Berke, S.*, Schirrmacher, R. (2015). Recent Advances in the Development and Application of Radiolabeled Kinase Inhibitors for PET Imaging. Molecules. 9(20): 22000-27.


Bernard-Gauthier, V.*, Bailey, J.J.*, Aliaga, A., Kostikov, A., Rosa-Neto, P., Wuest, M., Brodeur, G.M., Wuest, F., Schirrmacher, R. (2015). Development and first in vitro evaluation of fluorinated (2-pyrrolidin-1- yl)imidazo[1,2-b]pyridazine pan inhibitors as candidate PET imaging radioligands. MedChemComm (HOT article). 6: 2184-93.


Bernard-Gauthier, V.*, Aliaga, A., Aliaga, A., Boujemeline, M.*, Hopewell, R., Kostikov, A., Rosa-Neto, P., Thiel, A., Schirrmacher, R. (2015). Syntheses and evaluation of carbon-11 and fluorine-18 radiolabeled pan-tropomyosin receptor kinase (Trk) inhibitors: exploration of the 4-aza-2-oxindole scaffold as trk PET imaging agents. ACS Chem. Neuroscience. 6(2): 260-276.


Bernard-Gauthier, V.*, Schirrmacher, R. (2014). 5-(4-((4-[18F]fluorobenzyl)oxy)-3- methoxybenzyl)pyrimidine-2,4-diamine: A selective dual inhibitor for potential PET imaging of Trk/CSF-1R. Bioorg. Med. Chem. Lett. 15: 4784-4790.

Publications SiFA

Bernard-Gauthier, V.*; Lepage, M.; Waengler, B., Bailey, J. J.*; Liang, S. H.; Perrin, D.; Vasdev, N.; Schirrmacher, R. (2018). Recent advances in fluorine-18 radiochemistry: Focus on B-18F, Si-18F, Al-18F and C-18F radiofluorination via spirocyclic iodonium ylides. J Nucl Med. 59(4): 568-572.


Berke S*, Kampmann AL*, Wuest M, Bailey JJ*, Glowacki B, Wuest F, Jurkschat K, Weberskirch R, Schirrmacher R. (2017). 18F Radiolabeling and in vivo analysis of SiFA-derivatized polymeric core-shell nanoparticles. Bioconjugate Chemistry. 29(1): 1-11.


Bernard-Gauthier, V.*, Bailey, J.J.*, Liu, Z., Wängler, B., Wängler, C., Jurkschat, K., Perrin, D.M., Schirrmacher, R. (2016). From Unorthodox to Established: The Current Status of 18F-Trifluoroborate- and 18F-SiFA-Based Radiopharmaceuticals in PET Nuclear Imaging. Bioconjugate Chem. 27(2): 267-279.


Zhu, J.*, Li, S., Wängler, C., Wängler, B., Lennox, R.B., Schirrmacher, R. (2015). Synthesis of 3-chloro-6- ((4-(di-tert-butyl[18F]fluorosilyl)-benzyl)oxy)-1,2,4,5-tetrazine ([18F]SiFA-OTz) for Rapid Tetrazine-Based 18F-Radiolabeling. Chem. Comm.51: 12415-12418.


Niedermoser, S., Chin, J.*, Waengler, C., Kostikov, A., Bernard-Gauthier, V.*, Vogler, N., Soucy, J.P., McEwan, A.J., Schirrmacher, R., Waengler, B. (Schirrmacher and Waengler contributed equally and share last authorship). (2015). In vivo evaluation of 18F-SiFAlin modified TATE: A potential challenge for 68Ga-DOTATATE, the clinical gold standard for somatostatin receptor imaging with positron emission tomography (PET). Journal Nuclear Medicine. 56(7): 1100-5.


Litau, S., Niedermoser, S., Vogler, N., Roscher, M., Schirrmacher, R., Fricker, G., Wängler, B., Wängler, C. (2015). Next generation of SiFAlin-based TATE derivatives for PET imaging of SSTR-positive tumors: Influence of molecular design on in vitro SSTR binding and in vivo pharmacokinetics.. Bioconjugate Chem.26(12): 2350-9.


Bernard-Gauthier, V.*, Waengler, C., Schirrmacher, E., Kostikov, A., Jurkschat, K., Waengler, B., Schirrmacher, R. (2014). 18F-Labeled silicon-based fluoride acceptors-potential opportunities for novel positron emitting radiopharmaceuticals. Journal BioMed Research International http:// 2014


Zhu, J.*, Chin, J.*, Wängler, C.*, Waengler, B., Lennox, R.B., Schirrmacher, R. (2014). Rapid 18F-labeling and loading of PEGylated gold nanoparticles for in vivo applications. Bioconjugate Chem.25(6): 1142-1150.


Koudih, R.*, Kostikov, A., Kovacevic, M., Jolly, D., Bernard-Gauthier, V.*, Chin, J.*, Jurkschat, K., Wängler, C, Wängler, B., Schirrmacher, R. (2014). Automated radiosynthesis of N-succinimidyl 3-(di-tertbutyl[(18)F]fluorosilyl)benzoate ([(18)F]SiFB) for peptides and proteins radiolabeling for positron emission tomography. Int. J. Appl. Radiat Isot.89: 146-150.


Zhu, J.*, Hiltz, J., Mezour, M.A., Bernard-Gauthier, V.*, Lennox, R.B., Schirrmacher, R. (2014). Facile covalent modification of a highly ordered pyrolytic graphite (HOPG) surface via inverse electron demand Diels-Alder Reaction. Chem. Mater.26(17): 5058-5062.


Lindner, S., Michler, C., Leidner, S., Rensch, C., Wängler, C., Schirrmacher, R., Bartenstein, P., Wängler, B. (2014). Synthesis and in Vitro and in Vivo Evaluation of SiFA-Tagged Bombesin and RGD Peptides as Tumor Imaging Probes for Positron Emission Tomography. Bioconjugate Chem.16(4): 738-749.


Zhu, J.*, Hiltz, J., Lennox, R.B., Schirrmacher, R. (2013). Chemical modification of single walled carbon nanotubes with tetrazine-tethered gold nanoparticles via a Diels-Alder reaction. Chem. Comm.49(87): 10275-10277.


Kostikov, A.P.*, Chin, J.*, Orchowski, K.*, Schirrmacher, E., Niedermoser, S., Jurkschat, K., Iovkova- Berends, L., Wängler, C., Wängler, B., Schirrmacher, R. (2012). Synthesis of [(18)F]SiFB: a prosthetic group for direct protein radiolabeling for application in positron emission tomography. Nat. Protoc.7(11): 1956-1963.


Kostikov, A.P.*, Chin, J.*, Orchowski, K.*, Niedermoser, S., Kovacevic, M.M., Aliaga, A., Jurkschat, K., Wängler, B., Wängler, C.*, Wester, H.J., Schirrmacher, R. (2012). Oxalic acid supported Si-18Fradiofluorination: one-step radiosynthesis of N-succinimidyl 3-(di-tert-butyl[18F]fluorosilyl)benzoate ([18F]SiFB) for protein labeling. Bioconjugate Chem.23(1): 106-114.


Wängler, B., Kostikov, A.P.*, Niedermoser, S., Chin, J.*, Orchowski, K.*, Schirrmacher, E., Iovkova- Berends, L., Jurkschat, K., Wängler, C.*, Schirrmacher, R. (2012). Protein labeling with the labeling precursor [(18)F]SiFA-SH for positron emission tomography. Nat. Protoc.7(11): 1964-1969.


Wängler, C.*, Niedermoser, S., Chin, J.*, Orchowski, K.*, Schirrmacher, E.*, Jurkschat, K., Iovkova- Berends, L., Kostikov, A.P.*, Schirrmacher, R., Wängler, B. (2012). One-step (18)F labeling of peptides for positron emission tomography imaging using the SiFA methodology. Nat. Protoc.7(11): 1946-1955.


Kostikov, A.*, Iovkova, L., Chin, J.*, Schirrmacher, E., Waengler, B., Waengler, C.*, Jurkschat, K., Cosa,, Schirrmacher, R. (2011). N-(4-(di-tert-butyl[18F]fluorosilyl)benzyl)-2-hydroxy-N,N-dimethylethylammonium bromide: A novel lead compound for the development of hydrophilic SiFA-based prosthetic groups for 18Flabeling. J Fluorine Chem.132(1): 27-34.


Iovkova-Berends, L., Wängler, C.*, Zöller, T., Höfner, G., Wanner, K.T., Rensch, C., Bartenstein, P., Kostikov, A.*, Schirrmacher, R., Jurkschat, K., Wängler, B. (2011). t-Bu2SiF-derivatized D2-receptor ligands: the first SiFA-containing small molecule radiotracers for target-specific PET-imaging. Molecules.16(9): 7458-7479.


Wängler, C.*, Waser, B., Alke, A., Iovkova, L., Buchholz, H.G., Niedermoser, S., Jurkschat, K., Fottner, C., Bartenstein, P., Schirrmacher, R., Reubi, J.C., Wester, H.J., Wängler, B. (2010). One-step ¹⁸F-labeling of carbohydrate-conjugated octreotate-derivatives containing a silicon-fluoride-acceptor (SiFA): in vitro and in vivo evaluation as tumor imaging agents for positron emission tomography (PET). Bioconjugate Chem.21(12): 2289-2296.


Wängler B , Quandt G , Iovkova L , Schirrmacher E , Wängler C , Boening G , Hacker M , Schmoeckel M ,Jurkschat K , Bartenstein P , Schirrmacher R. (2009). Kit-like 18F-labeling of proteins: synthesis of 4-(ditert-butyl[18F]fluorosilyl)benzenethiol (Si[18F]FA-SH) labeled rat serum albumin for blood pool imaging with PET. Bioconjugate chemistry. 20(2)


Iovkova L , Wängler B , Schirrmacher E , Schirrmacher R , Quandt G , Boening G , Schürmann M ,Jurkschat K. (2009). para-Functionalized aryl-di-tert-butylfluorosilanes as potential labeling synthons for (18)F radiopharmaceuticals. Chemistry (Weinheim an der Bergstrasse, Germany). 15(9)


Schirrmacher E , Wängler B , Cypryk M , Bradtmöller G , Schäfer M , Eisenhut M , Jurkschat K ,

Schirrmacher R. (2007). Synthesis of p-(di-tert-butyl[(18)F]fluorosilyl)benzaldehyde ([(18)F]SiFA-A) with high specific activity by isotopic exchange: a convenient labeling synthon for the (18)F-labeling of N-aminooxy derivatized peptides. Bioconjugate chemistry. 18(6).


Schirrmacher R , Bradtmöller G , Schirrmacher E , Thews O , Tillmanns J , Siessmeier T , Buchholz HG , Bartenstein P , Wängler B , Niemeyer CM , Jurkschat K. (2006). 18F-labeling of peptides by means of an organosilicon-based fluoride acceptor. Angewandte Chemie (International ed. in English). 45(36).

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